Dosing and uses of Nicotrol NS (nicotine intranasal)
Adult dosage forms and strengths
intranasal spray
- 0.5mg/actuation
Smoking Cessation
Nicotine replacement therapy to reduce withdrawal symptoms during smoking cessation
1 spray/nostril (ie, 2 sprays to provide 1 mg/dose); typically 10-12 sprays/day in each nostril PRn
Initiate with 1-2 doses/hr; for greatest success, instruct patient to use at least 8 doses/day initially
Depending on individual addiction; may increase up to maximum dose of 40 mg (80 sprays/day)
Administration
Tilt head back when administering
Do not sniff, swallow, or inhale through the nose as the spray is being administered
Pediatric dosage forms and strengths
Safety and efficacy not established
Nicotrol NS (nicotine intranasal) adverse (side) effects
>10%
Local irritation (94%)
1-10%
Anxiety
Irritability
Restlessness
Cravings
Dizziness
Impaired concentration
Weight increase
Emotional lability
Somnolence and fatigue
Increased sweating
Insomnia
Confusion
Depression
Apathy
Tremor
Increased appetite
Incoordination
Increased dreaming
Warnings
Contraindications
Hypersensitivity
Cautions
Irritating to nasal mucosa
Not studied in reactive airway disease; may cause bronchospasm
Caution with hypertension, cardiovascular, or peripheral vascular disease
Caution with hyperthyroidism, pheochromocytoma, or insulin-dependent diabetes, since nicotine causes the release of catecholamines by the adrenal medulla
Delays healing of peptic ulcer disease
Pregnancy and lactation
Pregnancy category: d
Lactation: Distributed in breast milk; milk to plasma ratio is 2.9
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 Nicotrol NS (nicotine intranasal)
Mechanism of action
Agonist at nicotinic receptors
Absorption
Bioavailability: 53%
Peak plasma time: 4-15 minutes
Peak plasma concentration: 2-12 ng/mL
Absorption half-life: 3 minutes
Distribution
Protein bound: <5%
Vd: 2-3 L/kg
Metabolism
Metabolized primarily in the liver; some metabolism also takes place in kidney and lungs
More than 20 metabolites of nicotine identified, all are less active than the parent compound
The primary urinary metabolite is cotinine (15% of the dose)
Elimination
Half-life: 1-2 hr (nicotine); 15-20 hr (cotinine)
Plasma clearance: 1.2 L/min
Excretion: Urine (10-30% unchanged)
