Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2014 Publisher: Aurum Pharmaceuticals Ltd, Bampton road, Harold hill, Romford, Essex, RM3 8UG
Cocaine Hydrochloride Solution is indicated to provide local anaesthesia and vasoconstriction of accessible mucous membranes prior to surgery especially in the oral, laryngeal, and nasal cavities. Vasoconstriction prevents excessive blood loss and reduces obstruction/restriction of the operative field.
For topical use only. Not for injection or to be taken.
The maximum total dose recommended for application to the mucosa in fit adults is 1.5mg/Kg.
It should be used only by those skilled in the precautions needed to minimise absorption and the consequent risk of arrhythmias.(see section on Precautions)
Prime the pump dispenser by activating the pump 3 times.
The concentration of the cocaine hydrochloride solution is 100mg/ml. The dispenser contains only 2.5ml of solution.
One spray delivers 130µl of solution (containing 13mg of Cocaine). Therefore, a maximal dose of 1.5mg/Kg of cocaine (approx. 1ml of 10% solution), is equivalent to approximately 8-9 sprays for a 70Kg adult, and this dose must not be exceeded.
Any remaining solution should be returned to the pharmacy.
Cocaine hydrochloride solution should not be administered to children .
Cocaine hydrochloride solution should not be administered to the elderly .
Indications from some studies of medicinal cocaine show that death can ensue from 0.8-1.0g (8-10ml of a 10% w/v solution of cocaine).
Some persons have a cocaine idiosyncrasy and death may occur quite suddenly after doses of only 20mg.
The patient must be monitored for any signs or symptoms of toxicity during and after administration of cocaine. The appropriate treatment must be available and medical equipment must be ready for use at all times.
The signs and symptoms of overdose must be known to the otolaryngologist or anaesthetist administering cocaine topically.
Toxicity first occurs as an overstimulated excited state. The toxic reaction may progress to convulsions, loss of consciousness, respiratory and cardiovascular depression or arrest, and death.
Toxicity may arise from any route of cocaine administration. Clinically, otolaryngologists reported a higher percentage of untoward reactions when cocaine was applied to the tracheobronchial tree rather than the nasal mucosa.
Symptoms of acute toxicity include delirium, tremor, massive convulsions and a direct cardiotoxic effect due to its sympathomimetic effect.
Controlled clinical studies have been performed examining the dose-response effects from intranasal (snorting) administration of cocaine. At 10mg no observable subjective or physiological effects were apparent; at 25mg there was an increase in systolic blood pressure and mild euphoria reported as relaxation; at 100mg, heart rate and diastolic blood pressure were increased and a strong feeling of euphoria was present. These effects were short-lasting and lethargy and irritability as an after-effect were reported by a few subjects within one hour after a cocaine administration.
The LD50 (lethal dose that is fatal in 50% of cases) of cocaine in adults is estimated to be 500mg after oral administration.
A fatal dose of cocaine is about 0.8-1g for an adult. This is the amount contained in 8-10ml of a 10% w/v cocaine solution. This must be emphasised in order to appreciate the potency and danger of this cocaine solution.
On an acute basis, cocaine can prolong the time to reach orgasm in men and women.
Cocaine use by pregnant women can interfere with gestation and produce abnormalities, possibly permanent, in their children. (See Pregnancy And Lactation)
At clinical doses, cocaine has little general toxicity, when applied locally and for a short period of time.
If a cocaine-impregnated pledget is still in the nose when toxicity occurs, it must be promptly removed. Seizures, and cardiovascular and respiratory collapse in the late stages have been treated with respiratory support, anti-convulsants, and cardiotonic drugs.
The treatment of acute poisoning by cocaine should include the removal of any remaining drug from the mucosal surface by rinsing with tap water or normal saline.
In a medical setting where cocaine is used, positive-pressure breathing equipment should be functional and easily accessible, and intravenous diazepam should be immediately available.
Intravenous pentobarbital is a more stable preparation; it is slower acting but can be used if diazepam is not available.
Steps in the Management of Cocaine Overdose:
Prevent convulsion: At first sign of excitability (talkative stage), administer: diazepam injectable 5mg/ml 1-2ml intravenously in patients aged 5 years to adult
Hypertension: labetalol, phentolamine or sodium nitroprusside (not propranolol since it potentiates cocaine toxicity – see below*)
Psychiatric reactions: Delusions may respond to neuroleptics (phenothiazine and butyrophenone) but these agents also may increase the chance of seizures; benzodiazepines may be useful in reducing anxiety.
Respiratory support: After convulsion or if apnoeic or if Cheyne-Stokes respiration: Positive pressure ventilation – mouth to mouth, bag and mask, endotracheal
Cardiac resuscitation and anti-arrhythmics: In massive overdosage
* Propranolol has been used to treat cocaine-induced hypertension and arrhythmias but, following a report of paradoxical hypertension presumably due to unopposed α-adrenergic stimulation, a beta-blocker with both α- and β-adrenergic effects such as labetalol is now preferred by some for hypertension; sodium nitroprusside, or phentolamine may also be used.
However, one must be aware that like propranolol, labetalol may worsen hypertension in patients with hyperadrenergic states, because the β-blocking properties of labetalol are much more potent than its α-blocking properties. Like propranolol, labetalol has the potential to cause a state of relatively unopposed α-effect, thereby raising the blood pressure. If such a complication ensues, treatment with a pure α-blocker such as phentolamine, or a vasodilator such as nitroprusside, diazoxide, or possibly nifedipine is indicated. It has been found that esmolol, an ultra short-acting β1-selective adrenergic blocker with an elimination half-life of about 9 minutes, is an attractive choice for the treatment of a cocaine-induced hyperadrenergic state, because the β1-selectivity rendered hypertension or coronary artery spasm from unopposed α-adrenergic tone is less of a risk than with non-selective β-blocking drugs.
Shelf life: 1 year.
Do not store above 25°C. Protect from light. Store in the original container and keep in the outer case.
8ml type 1 clear glass bottle, with chlorobutyl rubber stopper and plastic screw cap, containing 2.5ml of a 10% w/v Cocaine Hydrochloride solution for topical application.
Ensure the dose used for each patient does not exceed 1.5mg/Kg (a volume of approximately 1ml, of a 10% w/v solution for a 70Kg adult). Any remaining solution must be returned to the pharmacy for disposal in the appropriate manner.
Not for multi-dose use.
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