COCAINE HYDROCHLORIDE

For topical use only. Not for injection or to be taken. 5mg/Kg. (see section on Precautions) Method of Administration Adults Prime the pump dispenser by activating the pump 3 times. The concentration of the cocaine hydrochloride solution is 100mg/ml.

5ml of solution. One spray delivers 130μl of solution (containing 13mg of Cocaine). 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.

Children Cocaine hydrochloride solution should not be administered to children . Elderly Cocaine hydrochloride solution should not be administered to the elderly . 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.

Cocaine may cause restlessness, excitement, euphoria, garrulousness and increased motor activity. With high doses or repeated use, confusion, paranoia, hallucinations, altered tactile sensations and psychosis have been reported. Seizures can occur, perhaps due to lowering of the seizure threshold, or hyperpyrexia, or due to life threatening cardiac arrhythmias.

Cocaine directly causes a rise in body temperature by increasing heat production through stimulated muscle activity, and indirectly by causing vasoconstriction that decreases heat loss. A direct pyrogenic effect may be caused by cocaine’s direct effect on thermoregulatory centres in the hypothalamic area.

Low doses of cocaine in humans do not change respiratory rate or depth, but at higher doses a CNS mediated increase in respiratory rate and decrease in tidal volume is described. A migraine-like headache may be the result of cocaine induced vascular changes.

Adrenergic stimulation may cause intensive hypertension, due to tachycardia and peripheral vasoconstriction. Cocaine increases cardiac activity, which raises oxygen demand within myocardial tissue. Other signs of adrenergic excess seen with cocaine include mydriasis, diaphoresis, tremor, hyperactive bowel sounds and hyperreflexia.

Vasoconstriction due to cocaine may also produce ischaemia in the fingers, toes, spinal cord, kidneys, spleen, and intestines. Cocaine suppresses Rapid Eye Movement (REM) sleep and total sleep. In low doses cocaine has an anorexic effect.

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. Cocaine should not be applied to damaged mucosa or open wounds because of the risk of systemic toxicity from enhanced absorption.

Cocaine should be used with caution in patients with hypertension, cardiovascular disease or thyrotoxicosis because the vasoconstriction and tachycardia may reduce cardiac oxygenation while increasing oxygen demand It should also be used with caution in patients with diabetes because cocaine sensitises the person to adrenaline which mobilises glucose and causes blood glucose levels to go out of control.

g. opiates, barbiturates, alcohol). The use of cocaine in the elderly is not recommended because of the risk of vasoconstriction and tachycardia. Cocaine is also not recommended in children, or in pregnancy or lactation. Overall, the patient’s condition, the appropriate dose and method of administration must all be considered prior to the application of cocaine.

The initial signs and symptoms of cocaine toxicity and the appropriate treatment required to combat toxicity must be known to the surgeon or anaesthetist.

Cocaine hydrochloride is largely (90%) metabolised by cholinesterase, thus those patients taking cholinesterase inhibitors such as Ecothiopate eye drops for the treatment of glaucoma, or neostigmine for the treatment of Myasthenia Gravis, or those patients with hereditary Pseudocholinesterase deficiency, should not be administered cocaine hydrochloride.

If these patients are given cocaine hydrochloride, higher blood levels result, with a greater risk of drug toxicity. Adrenaline is believed to enhance the toxic effects of cocaine by further increasing the level of circulating catecholamines, and thus should not be used in association.

Other sympathomimetic drugs are thus also contra-indicated. Cocaine hydrochloride’s use is also contra-indicated in patients receiving α- modifying drugs such as guanethidine sulphate, reserpine and tricyclic anti- depressants; as these drugs also increase the activity of the sympathetic nervous system.

Cocaine is contra-indicated in patients with epilepsy because it lowers the seizure threshold. Cocaine should be avoided in Porphyria, as it has been shown to be porphyrinogenic in animals or in vitro systems, thus exacerbating the disorder.