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alfentanil (Alfenta, Rapifen)

 

Classes: Synthetic, Opioids; Opioids, Anilidopiperidine

Dosing and uses of Alfenta, Rapifen (alfentanil)

 

Adult dosage forms and strengths

injectable solution: Schedule II

  • 0.5mg/mL

Dose should be calculated based on ideal body weight

 

Incremental Injection: Anesthesia <30 Minutes

Induction: 8-20 mcg/kg IV

Maintenance: 3-5 mcg/kg IV increments q5-20min, or 0.5-1 mcg/kg/min IV

Total dose: 8-40 mcg/kg IV

 

Incremental Injection: Anesthesia 30-60 Minutes

Induction: 20-50 mcg/kg IV

Maintenance: 5-15 mcg/kg IV increments q5-20min

Total dose: Up to 75 mcg/kg IV

 

Anesthetic Induction: Anesthesia >45 Minutes

Induction: 130-245 mcg/kg IV

Maintenance: 0.5-1.5 mcg/kg/min IV or other general anesthetic

Total dose: depends on duration of operation

 

Continuous Infusion: For Anesthesia >45 Minutes

Induction: 50-75 mcg/kg IV

Maintenance: 0.5-3 mcg/kg/min IV

Total dose: depends on duration of operation

 

Postherpetic Neuralgia (Orphan)

Management of postherpetic neuralgia

Orphan indication sponsor

  • Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212

 

HIV-Associated Neuropathy (Orphan)

Treatment of painful HIV-associated neuropathy

Orphan indication sponsor

  • Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212

 

Administration

Total dose: depends on duration of operation

 

Pediatric dosage forms and strengths

injectable solution: Schedule II

  • 0.5mg/mL

Dose should be calculated based on ideal body weight

<12 years

Anesthesia

  • Not recommended

>12 years

Incremental Injection: Anesthesia <30 Minutes

  • Induction: 8-20 mcg/kg IV
  • Maintenance: 3-5 mcg/kg IV increments q5-20min, or 0.5-1 mcg/kg/min IV
  • Total dose: 8-40 mcg/kg IV  

Incremental Injection: Anesthesia 30-60 Minutes

  • Induction: 20-50 mcg/kg IV
  • Maintenance: 5-15 mcg/kg IV increments q5-20min
  • Total dose: Up to 75 mcg/kg IV

Anesthetic Induction: Anesthesia >45 Minutes

  • Induction: 130-245 mcg/kg IV
  • Maintenance: 0.5-1.5 mcg/kg/min IV or other general anesthetic
  • Total dose: depends on duration of operation

Continuous Infusion: For Anesthesia >45 Minutes

  • Induction: 50-75 mcg/kg IV
  • Maintenance: 0.5-3 mcg/kg/min IV
  • Total dose: depends on duration of operation

 

Alfenta, Rapifen (alfentanil) adverse (side) effects

>10%

Arrhythmia (14%)

Bradycardia (14%)

Chest wall rigidity (17%)

Hypertension (18%)

Nausea (28%)

Vomiting (18%)

Tachycardia (12%)

 

1-10%

Apnea (3-9%)

Blurred vision (1-3%)

Dizziness (3-9%)

Hypotension (10%)

Post-op respiratory depression (1-3%)

Skeletal muscle movements (3-9%)

Postoperative sedation (1-3%)

 

<1%

Sweating, flushing

Warmness of the face/neck/upper thorax

Pruritus

urticaria

 

Respiratory (undefined)

Respiratory/circulatory depression

Respiratory arrest

Shock

Cardiac arrest

 

Nervous System (undefined)

Dizziness

Visual disturbances

Mental clouding/depression

Sedation

Coma

Euphoria

Dysphoria

Weakness

Faintness

Agitation

Restlessness

Nervousness

Seizures

 

GI (undefined)

Nausea

Vomiting

Constipation

 

Cardiovascular (undefined)

QT-interval prolongation

Severe cardiac arrhythmias

Cardiac arrest

ST segment elevation

VTach

MI

Angina pectoris

Syncope

 

Genitourinary (undefined)

Urinary retention

Oliguria

 

Cholinergic (undefined)

Bradycardia

Dry mouth

Palpitation

Tachycardia

 

Warnings

Contraindications

Hypersensitivity

Increased intracranial pressure

Severe respiratory depresssion

 

Cautions

Use caution in bradycardia, compromised cardiac reserve, head injury, hypothyroidism, increased ICP, intracranial lesions, renal impairment, respiratory impairment, obesicty, history of drug abuse

Concurrent administration of benzodiazepine or neuromuscular blocker will decrease chest wall rigidity

Skeletal muscle and chest wall rigidity, respiratory distress, or impaired ventilation may occur with rapid infusion (slow injection over 3-5min recommended)

Should be administered by trained individuals

 

Pregnancy and lactation

Pregnancy category: C

Lactation: use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Alfenta, Rapifen (alfentanil)

Mechanism of action

Narcotic agonist analgesic; increases pain threshold, inhibits ascending pain pathways, alters pain perception

 

Pharmacokinetics

Half-life: 5.33-8.75 hr (prematures, newborns); 40-60 min (children); 83-97 min (adults)

Onset: Immediate

Duration: 30-60 min

Vd: 1 L/kg (premature, newborns); 0.163-0.48 L/kg (children); 0.46 L/kg (adults)

Peak Plasma: distributed in decreasing order of concentration into skeletal muscle, kidneys, liver, intestinal tract, lungs, spleen, and brain

Bioavailability: Varies

Metabolism: liver (hepatic P450 enzyme CYP3A4), CNS, kidneys, lungs, and placenta (conjugation with glucuronic acid, hydrolysis, oxidation, N-dealkylation)

Excretion: urine, feces

 

Administration

IV Compatibilities

Solution: D5W

Syringe: atracurium, midazolam, ondansetron

Y-site: bivalirudin, cisatracurium, dexmedetomidine, etomidate, fenoldopam, gatifloxacin, Hextend, linezolid, propofol, remifentaniL

 

IV Incompatibilities

Y-site: amphotericin B cholSO4, thiopentaL

 

IV Preparation

Add 20 mL to 230 mL of diluent for a final concentration of 40 mg/mL

 

IV Administration

Keep Naloxone and resuscitation equip available

By incremental injection as analgesic adjunct to anesthesia with barbiturate/nitrous oxide/oxygen for short surgical procedures (expected duration <1 hr)

By continuous infusion as a maintenance analgesic with nitrous oxide/oxygen for general surgical procedures

By IV injection in aesthetic doses for anesthesia induction for general surgical procedures with a minimum expected duration of 45 min

By IV inj as the analgesic component for monitored anesthesia care (MAC)

 

Storage

Protect from light

Store at controlled room temp