Dosing and uses of Cocaine topical (cocaine)
Adult dosage forms and strengths
topical solution: Schedule II
- 4%
- 10%
Topical Anesthesia
As local anesthetic for accessible mucous membranes (oral, nasal and laryngeal)
1-10% solution: Use lowest dose necessary to produce adequate anesthesia
Do not exceed 1 mg/kg
Dosing Considerations
Dosage variables include tissue vascularity, anesthetic technique and patient tolerance
Reduce dose for elderly or debilitated patients
Administration
Administer using cotton applicators or packs, instilled into a cavity, or as a spray
Apply only on mucous membranes of mouth, laryngeal, or nasal cavities
Other Indications & Uses
Epistaxis (off-label)
Pediatric dosage forms and strengths
topical solution: Schedule II
- 4%
Topical Anesthesia
Use lowest possible effective dose; solutions >4% not recommended because of increased risk/severity of toxicity
Dosing Considerations
Dosage variables include tissue vascularity, anesthetic technique and patient tolerance
Administration
Administer using cotton applicators or packs, instilled into a cavity, or as a spray
Apply only on mucous membranes of mouth, laryngeal, or nasal cavities
Cocaine topical (cocaine) adverse (side) effects
Frequency not defined
Anxiety
Apprehension
Restlessness
Nervousness
Disorientation
Excitement
Confusion
Restlessness
Tremors, and possibly clonic-tonic convulsions
Respiratory arrest
Nausea
Vomiting
Chills
Miosis
Tinnitus
Myocardial depression
Bradycardia
Cardiac arrhythmias
Hypotension
Cardiovascular collapse
Cardiac arrest
Palpitation
Tachycardia
Anginal pain
Hypertension (epinephrine-containing solutions)
Sloughing of corneal epithelium (eg, pitting, clouding, corneal ulceration)
Serious toxic effects (eg, seizures, cardiac death) have been described following topical cocaine application used to anesthetize minor skin lacerations, especially on the face or scalp (eg, TAC [tetracaine 0.5%, epinephrine (Adrenalin) 1:2000, and cocaine 11.8%]); this risk is greater in pediatrics
Coronary arteriosclerosis
Tachyarrhythmia
Seizure
Edema
Status asthmaticus
Anaphylactoid reactions (sometimes fatal)
Warnings
Contraindications
Hypersensitivity to ester-type local anesthetics, para-aminobenzoic acid (PABA), or parabens
Cautions
Do not administer parenterally or apply to eye
Do not dilute with epinephrine for topical application as "cocaine mud"
Serious toxic effects (eg, seizures, cardiac death) have been described following topical cocaine application used to anesthetize minor skin lacerations, especially on the face or scalp (eg, TAC [tetracaine 0.5%, epinephrine (Adrenalin) 1:2000, and cocaine 11.8%]); this risk is greater in pediatrics
Pregnancy and lactation
Pregnancy category: C; X (nonmedicinal use)
Lactation: Enters breast milk; use is contraindicated
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 Cocaine topical (cocaine)
Mechanism of action
Acts as local anesthetic by blocking generation/conduction of nerve impulses by reducing sodium permeability and increasing action potential threshold
Absorption
Significant absorption from mucosa
Distribution
Protein Bound: High
Metabolism
Metabolism: Plasma esterases
Metabolites: Benzoylecgonine and ecgonine methyl ester (major)
Elimination
t1/2: 1 hr
Excretion: Urine (major)
