Dosing and uses of Fiorinal with Codeine (butalbital/aspirin/caffeine/codeine)
Adult dosage forms and strengths
butalbital/aspirin/caffeine/codeine
capsule: Schedule III
- 50mg/325mg/40mg/30mg
Tension Headache
1-2 tab/cap PO q4hr; not to exceed 6 tabs/caps per day
Pediatric dosage forms and strengths
capsule: Schedule III
- 50mg/325mg/40mg/30mg
Tension Headache
<16 years: Safety and efficacy not established
≥16 years: As adults; 1-2 tab/cap PO q4hr; not to exceed 6 tabs/caps per day
Geriatric dosage forms and strengths
Use caution; barbiturates not recommended in the elderly
Tension Headache
1-2 tab/cap PO q4hr; not to exceed 6 tabs/caps per day
Fiorinal with Codeine (butalbital/aspirin/caffeine/codeine) adverse (side) effects
>10%
Codeine
- Constipation
- Drowsiness
1-10%
Codeine
- Hypotension, tachycardia or bradycardia, confusion, dizziness, false feeling of well being, headache, lightheadedness, malaise, paradoxical CNS stimulation, restlessness, rash, urticaria, anorexia, nausea, vomiting, xerostomia, ureteral spasm, urination decreased, LFT's increased, weakness, blurred vision, dyspnea, histamine-release
Frequency not defined
ButalbitaL
- Drowsiness, sedation
- Lightheadedness, dizziness
- Shortness of breath
- Nausea, vomiting
- Abdominal pain
- Intoxicated feeling
Aspirin
- Stomach pain
- Heartburn
- Nausea, vomiting
- Dyspepsia
- Tinnitus (high or chronic dose)
- Rash
- Urticaria
Caffeine
- Insomnia, restlessness
- Nervousness, irritability
- Tremor
- Tinnitus
- Nausea, vomiting
- Diarrhea
- Tachycardia
Warnings
Black box warnings
Postoperative pain in children
- Deaths have occurred in children with obstructive sleep apnea who receive codeine for postoperative pain following tonsillectomy and/or adenoidectomy
- Codeine is converted to morphine by the liver; these children had evidence of being ultra-rapid metabolizers (via CYP2D6) of codeine, which is an inherited (genetic) ability that causes codeine to be converted rapidly into life-threatening or fatal amounts of morphine (see Pharmacology)
Contraindications
Hypersensitivity
Children younger than 16 years old because of potential for Reye syndrome
Postoperative use in children following tonsillectomy and/or adenoidectomy (see Black box warnings)
Bronchospastic reaction to aspirin
Peptic ulcer disease
Repeated administration in patients with anemia, cardiovascular, pulmonary, or renal disease
Porphyria
Cautions
Gastrointestinal bleeding; particular caution in patients with history of GI bleed, alcoholism, or bleeding disorders
Avoid driving car or operating machinery
Reye syndrome may occur in children because of aspirin component; do not use for chickenpox or flu symptoms
Avoid in severe renal impairment (ie, CrCl <10 mL/min)
May increase respiratory depressant effects; caution with head injury, COPD, or other conditions with decreased respiratory drive
Codeine may cause tolerance/dependency
Pregnancy and lactation
Pregnancy category: D; avoid during pregnancy, particularly in third trimester because of risk for premature closure of the ductus arteriosus because of aspirin component; codeine may prolong delivery and cause respiratory depression/withdrawal symptoms in newborn
Lactation: excreted in breast milk; do not breast feed
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 Fiorinal with Codeine (butalbital/aspirin/caffeine/codeine)
Mechanism of action
Butalbital: Barbiturate; elicits generalized CNS depressant effects
Aspirin: Acts on hypothalamus to produce antipyresis; anti-inflammatory properties attributed to prostaglandin synthetase inhibition resulting in decreased formation of thromboxane A2
Caffeine: Vasoconstrictive properties of cerebral blood vessels may be helpful when treating headaches
Codeine: Opioid agonist; analgesia
Pharmacogenomics
10% of codeine is metabolized to morphine by CYP2D6; the active morphine metabolite has a higher affinity for opioid receptors
CYP2D6 poor metabolizers may not achieve adequate analgesia
Ultra-rapid metabolizers (up to 7% of Caucasians and up to 30% of Asian and African populations) may have increased toxicity due to rapid conversion
